Patent SG-11201805838U-A (SG)
Title: Macrocyclic mcl1 inhibitors for treating cancer
Inventor: HIRD ALEXANDER
IPC: C07D515/22
Filed: 2017-04-21
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property 1 MI 11111 0 11101 HOE 010 1111 1 0 I OEM OH 1101 OHO 11110 MAMIE Organization International Bureau (10) International Publication Number (43) International Publication Date ......0\"\" WO 2017/182625 Al 26 October 2017 (26.10.2017) WIPO I PCT (51) International Patent Classification: AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, C07D 515/22 (2006.01) A61P 35/00 (2006.01) CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, A61K 31/395 (2006.01) DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, (21) International Application Number: HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KH, KN, KP, KR, PCT/EP2017/059511 KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, (22) International Filing Date: PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, 21 April 2017 (21.04.2017) SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (25) Filing Language: English (26) Publication Language: English (84) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, (30) Priority Data: GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, 62/326,156 22 April 2016 (22.04.2016) US UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, (71) Applicant: ASTRAZENECA AB [SE/SE]; SE-151 85 TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, Sodertalje (SE). MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, (72) Inventors: HIRD, Alexander; AstraZeneca 35 Gate- TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, house Drive, MA, Waltham 02451 (US). BELMONTE, KM, ML, MR, NE, SN, TD, TG). _ Matthew, Alan; AstraZeneca 35 Gatehouse Drive, MA, Waltham 02451 (US). YANG, Wenzhan; AstraZeneca Declarations under Rule 4.17: 35 Gatehouse Drive, MA, Waltham 02451 (US). SE- — as to applicant's entitlement to apply for and be granted a CRIST, John, Paul; AstraZeneca 35 Gatehouse Drive, patent (Rule 4.17(ii)) = MA, Waltham 02451 (US). ROBBINS, Daniel, William; Published: AstraZeneca 35 Gatehouse Drive, MA, Waltham 02451 — with international search report (Art. 21(3)) (US). KAZMIRSKI, Steven, Lee; AstraZeneca 35 Gate- — with sequence listing part of description (Rule 5.2(a)) house Drive, MA, Waltham 02451 (US). WU, Dedong; = — AstraZeneca 35 Gatehouse Drive, MA, Waltham 02451 = (US). PENG, Bo; AstraZeneca 35 Gatehouse Drive, MA, Waltham 02451 (US). JOHANNES, Jeffrey; AstraZeneca = 35 Gatehouse Drive, MA, Waltham 02451 (US). LAMB, Michelle, Laurae; AstraZeneca 35 Gatehouse Drive, MA, Waltham 02451 (US). YE, Oing; AstraZeneca 35 Gate- = = house Drive, MA, Waltham 02451 (US). ZHENG, Xi- _ aolan; AstraZeneca 35 Gatehouse Drive, MA, Waltham = 02451 (US). = (74) Agent: NESS, Mark; Milstein Building Granta Park, Cam- bridge Cambridgeshire CB21 6GH (GB). = (81) Designated States (unless otherwise indicated, for every = _ kind of national protection available): AE, AG, AL, AM, = Title: MACROCYCLIC MCL1 INHIBITORS FOR TREATING CANCER = (54) (57) : Disclosed is a compound which is 17-chloro-5,13,14,22-tetram- ethyl-28-oxa-2,9-dithia-5,6,12,13,22-pentaazaheptacyclo [27.7.1.14,7.011,15. _— 1-1 016,21.020,24.030,35]octatriaconta- 1(37),4(38),6,11,14,16,18,20,23,29,31,33,35-tride- fl caene-23-carboxylic acid (Formula I) and enantiomers and phar- in maceutically acceptable salts thereof. Also disclosed are phar- ei maceutical compositions of 17-chloro-5,13,14,22-tetramethy1-28-oxa-2,9- VZ+ ei ( 1 ) dithia- 5,6,12,13,22 -pentaazaheptacyclo [27.7.1.14,7.011,15.016,21.020,24.030,35]octatri- cc c OH aconta- 1(37),4(38),6,11,14,16,18,20,23,29,31,33,35 -tridecaene-23 -carboxylic acid, and 1-1 enantiomers and pharmaceutically acceptable salts thereof, and methods of treating cancer IN S N with such compounds and compositions. 1-1 N—N ei 0 O